Global Patent Index - EP 1188769 A3

EP 1188769 A3 20020710 - High resolution crystal structure of the ribosome and design of protein synthesis inhibitors

Title (en)

High resolution crystal structure of the ribosome and design of protein synthesis inhibitors

Title (de)

Kristallstruktur von Ribosomen und Proteinsynthese-Inhibitoren

Title (fr)

Structure cristallographique de Ribosome à haute résolution et inhibiteurs de la synthèse protéique

Publication

EP 1188769 A3 20020710 (EN)

Application

EP 01306825 A 20010809

Priority

  • US 63570800 A 20000809
  • US 22397700 P 20000809
  • US 30699601 P 20010720
  • US 30928101 P 20010801
  • US 92225101 A 20010803

Abstract (en)

[origin: EP1188769A2] The invention provides methods for producing high resolution crystals of ribosomes and ribosomal subunits as well as crystals produced by such methods. The invention also provides high resolution structures of ribosomal subunits either alone or in combination with protein synthesis inhibitors. The invention provides methods for identifying ribosome-related ligands and methods for designing ligands with specific ribosome-binding properties as well as ligands that may act as protein synthesis inhibitors. Thus, the methods and compositions of the invention may be used to produce ligands that are designed to specifically kill or inhibit the growth of any target organism.

IPC 1-7

C07K 14/215; G06F 17/50; G06F 19/00

IPC 8 full level

G01N 33/50 (2006.01); A61K 31/165 (2006.01); A61K 31/40 (2006.01); A61K 31/506 (2006.01); A61K 31/513 (2006.01); A61K 31/5355 (2006.01); A61K 31/7048 (2006.01); A61K 45/06 (2006.01); C07K 1/14 (2006.01); C07K 14/195 (2006.01); C07K 14/215 (2006.01); G01N 33/15 (2006.01)

CPC (source: EP US)

A61K 31/165 (2013.01 - EP US); A61K 31/40 (2013.01 - EP US); A61K 31/506 (2013.01 - EP US); A61K 31/513 (2013.01 - EP US); A61K 31/5355 (2013.01 - EP US); A61K 31/7048 (2013.01 - EP US); A61K 45/06 (2013.01 - EP US); A61P 31/04 (2017.12 - EP); C07K 14/215 (2013.01 - EP US); C07K 2299/00 (2013.01 - EP US)

Citation (search report)

  • [E] EP 1172374 A1 20020116 - MEDICAL RES COUNCIL [GB], et al
  • [XDY] CATE J H ET AL: "X-ray crystal structures of 70S ribosome functional complexes", SCIENCE, 24 SEPT. 1999, AMERICAN ASSOC. ADV. SCI, USA, vol. 285, no. 5436, pages 2095 - 2104, XP002193767, ISSN: 0036-8075
  • [XDY] BAN N ET AL: "Placement of protein and RNA structures into a 5 AA-resolution map of the 50 S ribosomal subunit", NATURE, 26 AUG. 1999, MACMILLAN MAGAZINES, UK, vol. 400, no. 6747, pages 841 - 847, XP002193768, ISSN: 0028-0836
  • [XD] BAN NENAD ET AL: "A 9 A resolution X-ray crystallographic map of the large ribosomal subunit.", CELL, vol. 93, no. 7, 26 June 1998 (1998-06-26), pages 1105 - 1115, XP002193769, ISSN: 0092-8674
  • [PXD] CLEMONS W M ET AL: "Structure of a bacterial 30S ribosomal subunit at 5.5 A resolution", NATURE, MACMILLAN JOURNALS LTD. LONDON, GB, vol. 400, 26 August 2000 (2000-08-26), pages 833 - 840, XP002182367, ISSN: 0028-0836
  • [A] AGALAROV S C ET AL: "Structure of the S15,S6,S18-rRNA complex: Assembly of the 30S ribosome central domain", SCIENCE, AMERICAN ASSOCIATION FOR THE ADVANCEMENT OF SCIENCE,, US, vol. 288, 7 April 2000 (2000-04-07), pages 107 - 112, XP002182369, ISSN: 0036-8075
  • [X] TOCILJ A ET AL: "The small ribosomal subunit from Thermus thermophilus at 4.5 A resolution: Pattern fittings and the identification of a functional site", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF USA, NATIONAL ACADEMY OF SCIENCE. WASHINGTON, US, vol. 96, no. 25, 7 December 1999 (1999-12-07), pages 14252 - 14257, XP002182368, ISSN: 0027-8424
  • [Y] HARMS JOERG ET AL: "Elucidating the medium-resolution structure of ribosomal particles: An interplay between electron cryo-microscopy and X-ray crystallography.", STRUCTURE (LONDON), vol. 7, no. 8, 15 August 1999 (1999-08-15), pages 931 - 941, XP002193770, ISSN: 0969-2126
  • [Y] MATADEEN RISHI ET AL: "The Escherichia coli large ribosomal subunit at 7.5 ANG resolution.", STRUCTURE (LONDON), vol. 7, no. 12, 15 December 1999 (1999-12-15), pages 1575 - 1583, XP002193771, ISSN: 0969-2126
  • [PX] SCHLUENZEN FRANK ET AL: "Structure of functionally activated small ribosomal subunit at 3.3 ANG resolution.", CELL, vol. 102, no. 5, 1 September 2000 (2000-09-01), pages 615 - 623, XP002193772, ISSN: 0092-8674
  • [PX] BAN N ET AL: "THE COMPLETE ATOMIC STRUCTURE OF THE LARGE RIBOSOMAL SUBUNIT AT 2.4 A RESOLUTION", SCIENCE, AMERICAN ASSOCIATION FOR THE ADVANCEMENT OF SCIENCE,, US, vol. 289, no. 5481, 11 August 2000 (2000-08-11), pages 905 - 920, XP001026334, ISSN: 0036-8075
  • [Y] SPAHN C M T ET AL: "THROWING A SPANNER IN THE WORKS: ANTIBIOTICS AND THE TRANSLATION APPARATUS", JOURNAL OF MOLECULAR MEDICINE, SPRINGER VERLAG, DE, vol. 74, no. 8, 1996, pages 423 - 439, XP000857835, ISSN: 0946-2716
  • [Y] DAVIES C ET AL: "RIBOSOMAL PROTEINS S5 AND L6: HIGH-RESOLUTION CRYSTAL STRUCTURES AND ROLES IN PROTEIN SYNTHESIS AND ANTIBIOTIC RESISTANCE", JOURNAL OF MOLECULAR BIOLOGY, LONDON, GB, vol. 279, no. 4, 19 June 1998 (1998-06-19), pages 873 - 888, XP001026810, ISSN: 0022-2836
  • [Y] HAASTRUP HANSEN L ET AL: "THE MACROLIDE-KETOLIDE ANTIBIOTIC BINDING SITE IS FORMED BY STRUCTURES IN DOMAINS II AND V OF 23S RIBOSOMAL RNA", MOLECULAR MICROBIOLOGY, BLACKWELL SCIENTIFIC, OXFORD, GB, vol. 31, no. 2, January 1999 (1999-01-01), pages 623 - 631, XP001055523, ISSN: 0950-382X
  • [Y] GSCHWEND D A ET AL: "MOLECULAR DOCKING TOWARDS DRUG DISCOVERY", JOURNAL OF MOLECULAR RECOGNITION, HEYDEN & SON LTD., LONDON, GB, vol. 9, 1996, pages 175 - 186, XP000882526, ISSN: 0952-3499
  • [Y] FITZHUGH A L: "Antibiotic inhibitors of the peptidyl transferase center. 1. Clindamycin as a composite analogue of the transfer RNA fragments L-Pro-Met and the D-ribosyl ring of adenosine", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 8, no. 1-6, 6 January 1998 (1998-01-06), pages 87 - 92, XP004136628, ISSN: 0960-894X
  • [A] RODRIGUEZ-FONSECA C ET AL: "FINE STRUCTURE OF THE PEPTIDYL TRANSFERASE CENTRE ON 23 S-LIKE RRNAS DEDUCED FROM CHEMICAL PROBING OF ANTIBIOTIC-RIBOSOME COMPLEXES", JOURNAL OF MOLECULAR BIOLOGY, LONDON, GB, vol. 247, no. 2, 24 March 1995 (1995-03-24), pages 224 - 235, XP000617137, ISSN: 0022-2836

Designated contracting state (EPC)

AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE TR

DOCDB simple family (publication)

EP 1188769 A2 20020320; EP 1188769 A3 20020710; EP 1188769 A8 20030903; EP 1188769 B1 20060524; AT E327250 T1 20060615; AU 5784601 A 20020214; AU 768033 B2 20031127; CA 2354051 A1 20020209; DE 01306825 T1 20050331; DE 60119853 D1 20060629; DE 60119853 T2 20070510; IL 144830 A0 20020630; JP 2003212896 A 20030730; JP 3836702 B2 20061025; US 2002086308 A1 20020704; US 2005234227 A1 20051020; US 2010131258 A1 20100527; US 6947844 B2 20050920

DOCDB simple family (application)

EP 01306825 A 20010809; AT 01306825 T 20010809; AU 5784601 A 20010807; CA 2354051 A 20010808; DE 01306825 T 20010809; DE 60119853 T 20010809; IL 14483001 A 20010809; JP 2001317401 A 20010808; US 22034208 A 20080722; US 91468004 A 20040809; US 92225101 A 20010803